在体内代谢和基于载体的药物相互作用与防晒活性成分的评估
Mohammed Qusa1, Hisham Qosa1,2, Donna A Volpe3
1Division of Applied Regulatory Science, Center for Drug Evaluation and Research, Food and Drug Administration, 10903 New Hampshire Ave., Silver Spring, MD, 20993-0002, USA.
Pharmaceutical research
|July 23, 2024
概括
防晒的成分,如氧松,经过药物相互作用的测试. 虽然有些人在实验室测试中抑制了药物代谢和运输,但在典型的防晒度下,它们对人体的影响不太可能.
科学领域:
- 药理学和毒理学 药理学和毒理学
- 皮肤病学 皮肤病学
- 药物代谢和运输 药物代谢和运输
背景情况:
- 防晒的活性成分广泛用于紫外线保护.
- 防晒成分与联合使用的药物之间的潜在相互作用令人担忧.
- 了解防晒对药物代谢和运输的影响对于消费者安全至关重要.
研究的目的:
- 评估六种防晒活性成分对细胞P450 (CYP) 酶的体外抑制潜力.
- 评估这些防晒成分对关键药物吸收输送器的功能的影响.
- 为了确定防晒的成分是否会干扰药物的新陈代谢和运输过程.
主要方法:
- 使用人类肝脏显微体进行的体外代谢测定用于CYP2C9,CYP2D6和CYP3A4.
- 在OAT3,OCT2和OATP1B1.1.的转染细胞系使用的体外吸收载体测定.
- 评估阿沃松,安扎卡门,氧松,奥克酸盐,托拉胺和同类盐到它们的可溶性极限.
主要成果:
- 恩扎卡门,氧和胺显示抑制CYP2C9活性,IC50值超过临床血水平.
- 对于任何测试的防晒成分,没有观察到对CYP2D6或CYP3A4的显著抑制.
- 氧化和胺抑制了OAT3和OCT2载体,但IC50值高于临床血度.
结论:
- 观察到一些防晒成分对CYP2C9和运输体进行了体外抑制.
- 测量到的IC50抑制值超过了临床研究中发现的血总水平.
- 这些防晒产品的活性成分不太可能抑制使用防晒产品的消费者药物代谢或运输.
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